Water soluble compositions and methods of making the same

Abstract

Provided is a composition for oral administration, the composition including: a dispersion medium including: an aqueous solution; and a dispersed phase including: a population of particles, each particle including: a core including: a first active ingredient; and an aqueous solution; a shell, substantially surrounding the core, the shell including: a lipophilic carrier; and a plurality of emulsifying agents; wherein the particle retards the release of the first active ingredient after consumption.

What is claimed is: 
     
       1. A composition for oral administration, the composition comprising:
 a dispersion medium comprising:
 an aqueous solution; and 
 
 a dispersed phase comprising:
 a population of particles, each particle comprising:
 a core comprising:
 a first active ingredient selected from the group consisting of methylphenidate, dextroamphetamine, amphetamine, Caffeine, nicotine, Methamphetamine, 3,4-Methylenedioxymethamphetamine, Methylenedioxypyrovalerone, Mephedrone, Phenylpropanolamine, Propylhexedrine, Pseudoephedrine, Catha  edulis , Modafinil, xanthines, theophylline, and theobromine; and 
 an aqueous solution; 
 
 a shell, at least substantially surrounding the core, the shell comprising:
 a lipophilic carrier selected from the group consisting of short-chain triglycerides, medium-chain triglycerides, long-chain triglycerides, medium-chain partial glycerides, polyoxyethylated fatty alcohols, polyethylene glycol, lemon oil, orange oil, peppermint oil, spearmint oil, Ylang Ylang oil, Lemon Grass oil, Tea Tree oil, Rosemary oil, Australian Sandalwood oil, Grape fruit oil, frankincense oil, cedarwood oil, patchouli oil, cinnamon bark oil, bergamot oil, chamomile oil, Lemon  Eucalyptus  oil, ginger oil, key lime oil,  vanilla  oil, vegetable oil, and combinations thereof; and 
 
 a plurality of emulsifying agents selected from the group consisting of an extract of  Quillaja , Tween 20, Tween 40, Tween 45, Tween 60, Tween 65, Tween 80, Tween 81 and Tween 85, polyglyceryl, gum  acacia , Polyglycerol polyricinoleate, Span 85, Span 65, Span 83, Span 80, Span 60, Span 40, Xanthan gum, sorbitol, mannitol, glycerol, sodium alginate, D-α-tocopheryl polyethylene glycol succinate, polyglycerols of oleic acid, and combinations thereof; 
 wherein the particle retards the release of the first active ingredient after consumption. 
 
 
 
     
     
       2. The composition of  claim 1 , wherein:
 the population of particles has a Z-average diameter less than 1 micron. 
 
     
     
       3. The composition of  claim 2 , wherein:
 the population of particles has a polydispersity of less than or equal to 0.25. 
 
     
     
       4. The composition of  claim 3 , wherein:
 the polydispersity of the population of particles changes by less than or equal to 100% upon 6 months of storage at 25° C. 
 
     
     
       5. The composition of  claim 4 , wherein:
 the storage is performed in an environment with 50% relative humidity. 
 
     
     
       6. The composition of  claim 3 , wherein:
 the polydispersity of the population of particles changes by less than or equal to 100% upon 30 minutes of storage at 85° C. 
 
     
     
       7. The composition of  claim 3 , wherein:
 the polydispersity of the population of particles changes by less than or equal to 20% upon pasteurization of the composition. 
 
     
     
       8. The composition of  claim 1  further comprising:
 a food additive polysaccharide; 
 a flavoring agent; and 
 a preservative agent. 
 
     
     
       9. The composition of  claim 1 , wherein the core further comprises:
 a first polymer selected from the group consisting of alginic acid, sodium alginate, potassium alginate, calcium alginate, agar, guar gum, and xanthan gum. 
 
     
     
       10. The composition of  claim 9 , wherein:
 the first polymer is a chelating agent for the first active ingredient. 
 
     
     
       11. The composition of  claim 1 , wherein the shell further comprises:
 a second polymer, wherein the second polymer is water insoluble and is selected from the group consisting of methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, shellac, ethyl methyl cellulose, carboxymethyl cellulose, ethyl cellulose, microcrystalline cellulose, cellulose, 12-hydroxystearic acid, and combinations thereof. 
 
     
     
       12. The composition of  claim 11 , wherein:
 the second polymer has a glass transition temperature above 120° C. 
 
     
     
       13. The composition of  claim 1 , wherein the shell further comprises:
 a second active ingredient, wherein the second active ingredient is selected from the group consisting of hemp,  cannabis, Echinacea purpurea, Echinacea angustifolia, Echinacea pallida, Acmella oleracea, Helichrysum umbraculigerum, Radula marginata , kava, black truffle,  Syzygium aromaticum, Rosmarinus  oficinalis, basil, oregano, lavender, true cinnamon, malabathrum,  cananga odorata , Riboflavin, Theanine,  Ginkgo Biloba , Bacopa,  Rhodiola Rosea  Extract, kanna, berberine, Lion's Mane, reishi mushroom, valerian root,  cordyceps , Maca, Passionflower, Saffron, Schisandra, St. John's Wort, Turmeric, Turkey Tail, Yohimbe, Ashwagandha,  Astragalus , Chaga and combinations thereof. 
 
     
     
       14. The composition of  claim 1 , wherein:
 at least 60% by weight of the first active ingredient is not released within 30 minutes after consumption; and 
 at least 80% by weight of the first active ingredient is not released within 2 hours after consumption. 
 
     
     
       15. The composition of  claim 1 , wherein:
 at least 10% by weight of the first active ingredient is not released within 6 hours after consumption. 
 
     
     
       16. The composition of  claim 1 , wherein:
 the shell do not break down in an aqueous solution with a pH above 5.5. 
 
     
     
       17. The composition of  claim 1 , wherein the shell further comprises:
 a wax is selected from the group consisting of bees wax, carnauba wax, rice bran wax, camauba wax, candelilla wax, or combinations thereof. 
 
     
     
       18. The composition of  claim 1 , wherein the shell further comprises:
 at least one source of bioavailibity enhancer selected from the group consisting of naringin, naringenin, piperine, capsaicin, curcumin, demethoxycurcumin, bis-demethoxycurcumin, quercetin, allicin, lysergol, genistein, sinomenine, gallic acid, glycodeoxycholic acid, docosahexaenoic acid, eicosapentaenoic acid, epicatechin, cyclosporine, diosmin, emodin, fulvic acid genistein, lycopene, trans-resveratrol cis-resveratrol, capric acid, cholic acid, deoxycholic acid, tamarixetin, glycocholic acid, taurocholic acid, limonene carvone, tangeretin, nobiletin, bergamottin, 6′,7′-dihydroxybergamottin, L-palmitoylcarnitine, and quinidine. 
 
     
     
       19. A composition for oral administration, the composition comprising:
 a dispersion medium comprising:
 an aqueous solution; and 
 
 a dispersed phase comprising:
 a population of particles, each particle comprising:
 a core comprising:
 a first active ingredient, wherein the first active ingredient is selected from the group consisting of methylphenidate, dextroamphetamine, amphetamine, Caffeine, nicotine, Methamphetamine, 3,4-Methylenedioxymethamphetamine, Methylenedioxypyrovalerone, Mephedrone, Phenylpropanolamine, Propylhexedrine, Pseudoephedrine, Catha  edulis , Modafinil, xanthines theophylline, and theobromine; and 
 an aqueous solution of a first polymer, the first polymer is selected from the group consisting of alginic acid, gum Arabic, locust bean gum, sodium alginate, potassium alginate, calcium alginate, agar, guar gum, and xanthan gum; 
 
 a shell, at least substantially surrounding the core, the shell comprising:
 a lipophilic carrier selected from the group consisting of short-chain triglycerides, medium-chain triglycerides, long-chain triglycerides, medium-chain partial glycerides, polyoxyethylated fatty alcohols, polyethylene glycol, lemon oil, orange oil, peppermint oil, spearmint oil, Ylang Ylang oil, Lemon Grass oil, Tea Tree oil, Rosemary oil, Australian Sandalwood oil, Grape fruit oil, frankincense oil, cedarwood oil, patchouli oil, cinnamon bark oil, bergamot oil, chamomile oil, Lemon  Eucalyptus  oil, ginger oil, key lime oil,  vanilla  oil, vegetable oil, and combinations thereof; 
 a second polymer, wherein the second polymer is water insoluble and is selected from the group consisting of methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, shellac, ethyl methyl cellulose, carboxymethyl cellulose, ethyl cellulose, microcrystalline cellulose, cellulose, 12-hydroxystearic acid, and combinations thereof; 
 a second active ingredient, wherein the second active ingredient is selected from the group consisting of  Echinacea Purpurea, Echinacea Angustifolia, Echinacea Pallida, Acmella Oleracea, Helichrysum Umbraculigerum, Radula Marginata , Kava, Kanna, black truffle,  Syzygium aromaticum, Rosmarinus  Oficinalis,  Sceletium Tortuosum , Holy basil, Oregano, Lavender, Cinnamon, Malabathrum,  Cananga odorata, Ginkgo Biloba , Bacopa,  Rhodiola rosea , Ashwagandha,  Astragalus, Chaga, Cordyceps, Corydalis , Curcumin, Damiana, Eleuthero, Ginger root,  Ginseng , Gotu Kola, Lion's Mane, Maca, Passionflower, Saffron, Schisandra, St. John's Wort, Turmeric, Turkey Tail, Valerian root, Yohimbe, cannabidiol, cannabichromene, cannabigerol, cannabicyclol, cannabinol, cannabigerolic acid, cannabigerolic acid monomethylether, cannabigerol monomethyl ether, cannabichromanon, cannabichromenic acid, cannabichromevarin, cannabichromevarinic acid, tetrahydrocannabinol, iso-tetrahydrocannabinol, cannabinol methylether, cannabinol-C4, cannabinol-C2, cannabiorcol, cannabinodiol, cannabielsoin, cannabielsoic acid A, cannabielsoic acid B, cannabicyclol, cannabicyclolic acid, cannabicyclovarin, cannabicitran, cannabitriol, cannabitriolvarin, ethoxy-cannabitiolvarin, cannabivarin, cannabinodivarin, tetrahydrocannabivarin, cannabidivarin, cannabigerovarin, cannabigerovarinic acid, cannabifuran, dehydrocannabifuran, cannabiripsol cannabinoids, Withaferin, Astragalosides, Bacoside, Betulinic Acid, Betulinic Acid, L-Tetrahydropalmatine, Dehydrocorybulbine, Apigenin, Eleutherosides, Gingerenone, Shogaol, Gingerol, Diterpenes, Ginkgetin, Bilobetin, Sciadopitysin, Ginsenoside, Eugenol, Mesembrine, Kavain, Hericenone, Erinacine, Macamides, Chrysin, Coumerin, Umbelliferone, Triterpenoids, Rhodiolin, Crocetin, Schisandrin A, Schisandrin B, Schisandrin C, Hypericin, Hyperforin, Valerenic Acid, Yohimbine, Melatonin, Vitamin A, Vitamin D3, Vitamin E, and Vitamin K; and 
 
 a plurality of emulsifying agents selected from the group consisting of an extract of  Quillaja , Tween 20, Tween 40, Tween 45, Tween 60, Tween 65, Tween 80, Tween 81 and Tween 85, polyglyceryl, gum  acacia , Polyglycerol polyricinoleate, Span 85, Span 65, Span 83, Span 80, Span 60, Span 40, Xanthan gum, sorbitol, mannitol, glycerol, sodium alginate, D-α-tocopheryl polyethylene glycol succinate, polyglycerols of oleic acid, and combinations thereof; 
 
 
 wherein:
 the particle is configured to retard the release of the first active ingredient after consumption; 
 the population of particles has a Z-average diameter less than 1 micron; and 
 the polydispersity of the population of particles changes by less than or equal to 100% upon 6 months of storage at 25° C. 
 
 
     
     
       20. A composition for oral administration, the composition comprising:
 a dispersion medium comprising:
 an aqueous solution; and 
 
 a dispersed phase dispersed in the dispersion medium, the dispersed phase comprising:
 a population of particles, each particle comprising:
 a core comprising:
 a first active ingredient, wherein the first active ingredient selected from the group consisting of caffeine, xanthines matcha extract, Citicoline Sodium, Phosphatidylserine, and L-Theanine; and 
 an aqueous solution of a first polymer, wherein the first polymer is selected from the group consisting of locust bean gum, sodium alginate, agar, and xanthan gum; 
 
 a shell, at least substantially surrounding the core, the shell comprising:
 a lipophilic carrier selected from the group consisting of selected from the group consisting of medium-chain triglycerides, long-chain triglycerides, and combinations thereof; 
 a second polymer, wherein the second polymer is water insoluble and is selected from the group consisting of methyl cellulose, ethyl cellulose, 12-hydroxystearic acid, and combinations thereof; 
 a second active ingredient, wherein the second active ingredient is selected from the group consisting of Kava, Kanna, Holy basil, Bacopa,  Rhodiola rosea , Ashwagandha,  Astragalus, Chaga, Cordyceps, Corydalis , Curcumin, Damiana, Eleuthero,  Ginseng , Lion's Mane, Maca, Passionflower, Schisandra, St. John's Wort, Turmeric, Turkey Tail, Valerian root, Yohimbe, cannabidiol, cannabinol, Vitamin A, Vitamin D3, Vitamin E, Vitamin B, and Vitamin K; and 
 
 a plurality of emulsifying agents selected from the group consisting of an extract of  Quillaja , Tween 80, Polyglycerol polyricinoleate, D-α-tocopheryl polyethylene glycol succinate, polyglycerols of oleic acid, and combinations thereof; 
 
 
 wherein:
 the population of particles has a Z-average diameter less than 1 micron; and 
 the polydispersity of the population of particles changes by less than or equal to 100% upon 6 months of storage at 25° C.